First synthesis of BU-4664L

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Abstract

The first synthesis of BU-4664L, an actinomycte-produced N-farnesylated dibenzodiazepinone with important biological activities, has been achieved in 18% overall yield from a known benzoic acid derivative by a nine-step sequence that involves an intramolecular Buchwald-Hartwig coupling of a sterically demanding bromo amine intermediate to install the unique tricyclic ring system.

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Takahashi, Y., Hirokawa, T., Watanabe, M., Fujita, S., Ogura, Y., Enomoto, M., & Kuwahara, S. (2015). First synthesis of BU-4664L. Tetrahedron Letters, 56(41), 5670–5672. https://doi.org/10.1016/j.tetlet.2015.08.070

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